Potent 4-aminopiperidine based antimalarial agents
KM Brinner, MA Powles, DM Schmatz…
Index: Brinner, Kristin M.; Powles, Mary Ann; Schmatz, Dennis M.; Ellman, Jonathan A. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 2 p. 345 - 348
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Citation Number: 13
Abstract
A series of compounds with potent activity against a multi-drug-resistant strain of Plasmodium falciparum, the causative agent of the deadliest strain of malaria, is described. These compounds were also tested for cytotoxicity in human foreskin fibroblast assays, evaluated to determine their logD, and assayed for metabolism by human and murine hepatocytes. This work resulted in the development of compounds 9e and 10d, which ...